| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
This study compared the dose-response of Chiglitazar with rosiglitazone and pioglitazone for PPARγ, and compared the dose-response of Chiglitazar with WY14643 for PPARα. The results showed that Chiglitazar had a significant activating effect on both subtypes. Chiglitazar's PPARγ activation activity was weaker than that of rosiglitazone, but stronger than that of pioglitazone. In terms of PPARα activation, Chiglitazar's activity was stronger than that of rosiglitazone, pioglitazone, and the selective PPARα agonist WY14643[1].
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|---|---|
| ln Vivo |
Following insulin injection, compared with the control group (injected excipient), MSG obese rats treated with ciglitazone or rosiglitazone showed significantly lower plasma glucose levels at all time points. The fasting insulin secretion index (PI) of the animals in the ciglitazone and rosiglitazone treatment groups was lower than that in the control group. The insulin sensitivity index (ISI) of the MSG obese rats in the ciglitazone and rosiglitazone treatment groups was significantly higher than that in the control group. In addition, ciglitazone improved the homeostasis model assessment of insulin resistance index (HOMA-IR). In the intraperitoneal glucose tolerance test (IPGTT), 30 minutes after glucose loading, the glucose values in the 5 mg/kg and 10 mg/kg ciglitazone and rosiglitazone treatment groups were significantly lower than those in the excipient group. The glucose response scores of the treatment groups during the IPGTT were significantly lower than those of the control group [2].
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| References |
| Molecular Formula |
C36H28FN2NAO4
|
|---|---|
| Molecular Weight |
594.61
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| CAS # |
2390374-10-2
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
O=C(C1=CC=C(C=C1)F)C(C=CC=C2)=C2N[C@H](C(O[Na])=O)CC(C=C3)=CC=C3OCCN4C5=CC=CC=C5C6=CC=CC=C64
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| Synonyms |
Carfloglitazar sodium
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6818 mL | 8.4089 mL | 16.8177 mL | |
| 5 mM | 0.3364 mL | 1.6818 mL | 3.3635 mL | |
| 10 mM | 0.1682 mL | 0.8409 mL | 1.6818 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.